EP3788055A4 - NEUROSTEROID DERIVATIVES AND USES THEREOF - Google Patents

NEUROSTEROID DERIVATIVES AND USES THEREOF Download PDF

Info

Publication number
EP3788055A4
EP3788055A4 EP19796480.2A EP19796480A EP3788055A4 EP 3788055 A4 EP3788055 A4 EP 3788055A4 EP 19796480 A EP19796480 A EP 19796480A EP 3788055 A4 EP3788055 A4 EP 3788055A4
Authority
EP
European Patent Office
Prior art keywords
neurosteroid
derivatives
neurosteroid derivatives
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP19796480.2A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP3788055A2 (en
Inventor
Nathan Bryson
Avinash Chander Sharma
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Acerus Pharmaceuticals Corp
Original Assignee
Acerus Pharmaceuticals Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Acerus Pharmaceuticals Corp filed Critical Acerus Pharmaceuticals Corp
Publication of EP3788055A2 publication Critical patent/EP3788055A2/en
Publication of EP3788055A4 publication Critical patent/EP3788055A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/009—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by only one oxygen atom doubly bound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/658—Medicinal preparations containing organic active ingredients o-phenolic cannabinoids, e.g. cannabidiol, cannabigerolic acid, cannabichromene or tetrahydrocannabinol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
    • C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Dispersion Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Inorganic Chemistry (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP19796480.2A 2018-05-04 2019-05-03 NEUROSTEROID DERIVATIVES AND USES THEREOF Withdrawn EP3788055A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862667100P 2018-05-04 2018-05-04
PCT/IB2019/000517 WO2019211668A2 (en) 2018-05-04 2019-05-03 Neurosteroid derivatives and uses thereof

Publications (2)

Publication Number Publication Date
EP3788055A2 EP3788055A2 (en) 2021-03-10
EP3788055A4 true EP3788055A4 (en) 2022-03-30

Family

ID=68384780

Family Applications (1)

Application Number Title Priority Date Filing Date
EP19796480.2A Withdrawn EP3788055A4 (en) 2018-05-04 2019-05-03 NEUROSTEROID DERIVATIVES AND USES THEREOF

Country Status (11)

Country Link
US (2) US20190337975A1 (https=)
EP (1) EP3788055A4 (https=)
JP (1) JP2021523938A (https=)
CN (1) CN112823164A (https=)
AR (1) AR116659A1 (https=)
AU (1) AU2019264032A1 (https=)
CA (1) CA3099089A1 (https=)
PY (1) PY1934080A (https=)
TW (1) TW202014192A (https=)
UY (1) UY38213A (https=)
WO (1) WO2019211668A2 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201606063RA (en) 2012-01-23 2016-09-29 Sage Therapeutics Inc Neuroactive steroid formulations and methods of treating cns disorders
MX2015002252A (es) 2012-08-21 2015-07-21 Sage Therapeutics Inc Metodos para tratar epilepsia o estado de epilepsia.
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
JP6470258B2 (ja) 2013-04-17 2019-02-13 セージ セラピューティクス， インコーポレイテッド １９−ノルｃ３，３−ジ置換ｃ２１−ｎ−ピラゾリルステロイドおよびその使用方法
ES2848823T3 (es) 2013-08-23 2021-08-12 Sage Therapeutics Inc Esteroides neuroactivos, composiciones y usos de los mismos
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
US10577390B2 (en) 2014-10-16 2020-03-03 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
ME03809B (me) 2014-10-16 2021-04-20 Sage Therapeutics Inc KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a
WO2016123056A1 (en) 2015-01-26 2016-08-04 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
HK1258616A1 (zh) 2016-03-08 2019-11-15 Sage Therapeutics, Inc. 神经活性类固醇、组合物、及其用途
US20190233465A1 (en) 2016-07-11 2019-08-01 Sage Therapeutics, Inc. C7, c12, and c16 substituted neuroactive steroids and their methods of use
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
CR20240234A (es) 2019-05-31 2024-07-09 Sage Therapeutics Inc ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629)
CN115348864A (zh) * 2020-02-05 2022-11-15 纯技术Lyt股份有限公司 神经甾体的脂质前药
MX2022010620A (es) * 2020-02-27 2022-11-30 Brii Biosciences Inc Profarmacos de esteroides neuroactivos.
IL315509A (en) * 2022-03-18 2024-11-01 Marinus Pharmaceuticals Inc Genaxolone medication matrims

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995021617A1 (en) * 1994-02-14 1995-08-17 Cocensys, Inc. Androstanes and pregnanes for allosteric modulation of gaba receptor
WO2012127176A1 (fr) * 2011-03-23 2012-09-27 Université De Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
WO2018237282A1 (en) * 2017-06-23 2018-12-27 The Board Of Trustees Of The University Of Illinois Treatment of neuropsychiatric disorders with neurosteroids and analogues thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB748846A (en) * 1953-10-28 1956-05-09 Vitamins Ltd A process for the manufacture of pregnan-3(-a)-ol-20-one and derivatives thereof
US5232917A (en) * 1987-08-25 1993-08-03 University Of Southern California Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series
US20060009432A1 (en) * 2004-07-09 2006-01-12 Roger Whiting Use of neurosteroids to treat neuropathic pain
WO2011120044A1 (en) * 2010-03-26 2011-09-29 Duke University Conjugated neuroactive steroid compositions and methods of use
US20170022245A1 (en) * 2013-11-26 2017-01-26 Biopharma Works Ganaxolone derivatives for treatment of central nervous systems disorders
CN109666055A (zh) * 2017-10-16 2019-04-23 张家口华健致远生物科技有限公司 调节中枢神经治疗抑郁症的化合物及其用途

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995021617A1 (en) * 1994-02-14 1995-08-17 Cocensys, Inc. Androstanes and pregnanes for allosteric modulation of gaba receptor
WO2012127176A1 (fr) * 2011-03-23 2012-09-27 Université De Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
WO2018237282A1 (en) * 2017-06-23 2018-12-27 The Board Of Trustees Of The University Of Illinois Treatment of neuropsychiatric disorders with neurosteroids and analogues thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JOHNSON FRANCIS ET AL: "Part XIII. The Conversion of Ergosterol into Progesterone.", JOURNAL OF THE CHEMICAL SOCIETY, 1 January 1954 (1954-01-01), pages 1302 - 1306, XP055890180, ISSN: 0368-1769, Retrieved from the Internet <URL:10.1039/jr9540001302> *

Also Published As

Publication number Publication date
WO2019211668A3 (en) 2019-12-12
TW202014192A (zh) 2020-04-16
EP3788055A2 (en) 2021-03-10
UY38213A (es) 2019-10-31
CA3099089A1 (en) 2019-11-07
AR116659A1 (es) 2021-06-02
PY1934080A (es) 2019-11-08
AU2019264032A1 (en) 2020-12-03
US20190337975A1 (en) 2019-11-07
JP2021523938A (ja) 2021-09-09
CN112823164A (zh) 2021-05-18
WO2019211668A2 (en) 2019-11-07
US20210363173A1 (en) 2021-11-25

Similar Documents

Publication Publication Date Title
EP3788055A4 (en) NEUROSTEROID DERIVATIVES AND USES THEREOF
EP3706762A4 (en) N4-HYDROXYCYTIDINE AND DERIVATIVES AND ANTIVIRAL USES IN RELATION TO IT
MA52483A (fr) Dérivés de gip et leurs utilisations
EP3841096A4 (en) PYRIDINYLMETHYLENEPIPERIDEINDIVATES AND THEIR USES
EP3908571A4 (en) KETAMINE DERIVATIVES AND COMPOSITIONS THEREOF
MA50256A (fr) Composés de pyrazolopyrimidinone et leurs utilisations
EP3787607C0 (en) CAROTINOID COMPOSITIONS AND USES THEREOF
EP3917529A4 (en) Compounds and uses thereof
EP3849983A4 (en) TRIAZOLEPYRIMIDINE COMPOUNDS AND USES THEREOF
EP3694861A4 (en) HETEROCYCLIC COMPOUNDS AND USES THEREOF
MA50618A (fr) Polyrhérapies et leurs utilisations
MA52365A (fr) Composés et leurs utilisations
EP3917527A4 (en) CONNECTIONS AND USES THEREOF
MA52092A (fr) Composés et leurs utilisations
MA55385A (fr) Composés et leurs utilisations
EP3829590A4 (en) LIPID PRODRUGS OF PREGNAN NEUROSTEROIDS AND THEIR USES
MA50413A (fr) Dérivés de benzimidazole et leurs utilisations
EP4017843A4 (en) Benzenesulfonamide derivatives and uses thereof
EP3790883A4 (en) Heteroaryl compounds and uses thereof
EP3526215A4 (en) N-ACYLETHANOLAMIDE DERIVATIVES AND USES THEREOF
EP3630154A4 (en) LIPO-GLYCOPEPTIDE Cleavable Derivatives and Uses Thereof
MA52411A (fr) Dérivés de 2,4-diaminoquinazoline et leurs utilisations médicales
MA52976A (fr) Dérivés de tétrahydrothiénopyridine n-substitués et leurs utilisations
EP3853216A4 (en) SUBSTITUTED PYRIDINYL COMPOUNDS AND USES THEREOF
EP3535243A4 (en) TRICYCLIC HETEROCYCLENE DERIVATIVES AND USE THEREOF

Legal Events

Date Code Title Description
STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE

PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: REQUEST FOR EXAMINATION WAS MADE

17P Request for examination filed

Effective date: 20201105

AK Designated contracting states

Kind code of ref document: A2

Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

AX Request for extension of the european patent

Extension state: BA ME

DAV Request for validation of the european patent (deleted)
DAX Request for extension of the european patent (deleted)
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40048529

Country of ref document: HK

A4 Supplementary search report drawn up and despatched

Effective date: 20220225

RIC1 Information provided on ipc code assigned before grant

Ipc: A61K 9/107 20060101ALI20220221BHEP

Ipc: A61K 47/02 20060101ALI20220221BHEP

Ipc: A61P 25/24 20060101ALI20220221BHEP

Ipc: A61K 47/14 20170101ALI20220221BHEP

Ipc: A61K 9/48 20060101ALI20220221BHEP

Ipc: A61K 31/05 20060101ALI20220221BHEP

Ipc: A61K 9/06 20060101ALI20220221BHEP

Ipc: A61K 9/00 20060101ALI20220221BHEP

Ipc: C07J 9/00 20060101ALI20220221BHEP

Ipc: C07J 5/00 20060101ALI20220221BHEP

Ipc: C07J 1/00 20060101ALI20220221BHEP

Ipc: A61K 47/44 20170101ALI20220221BHEP

Ipc: A61K 31/57 20060101ALI20220221BHEP

Ipc: C07J 7/00 20060101AFI20220221BHEP

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN

18D Application deemed to be withdrawn

Effective date: 20231201